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Tazemetostat

Inh 1403254-99-8 N-((4,6-Dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-5-(ethyl(tetrahydro-2H-pyran-4-yl)amino)-4-methyl-4'-(morpholinomethyl)-[1,1'-biphenyl]-3-carboxamide
Catalog No. ABIN7233296

Quick Overview for Tazemetostat (ABIN7233296)

Application

Inhibition (Inh)

Chemical Name

N-((4,6-Dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-5-(ethyl(tetrahydro-2H-pyran-4-yl)amino)-4-methyl-4'-(morpholinomethyl)-[1,1'-biphenyl]-3-carboxamide
  • Purpose

    EZH2 inhibitor

    Characteristics

    Potent and selective SAM-competitive inhibitor of the lysine methyltransferase EZH2 (Ki = 2.5nM wild type human PRC2-containing). Displayed strong antiproliferative effects against SMARCB1-deleted malignant rhabdoid tumor (MRT) cell lines in vitro. Antitumor activity was also observed in SMARTCB1 mutant mouse xenografts. Displays potent antitumor activity in various cancer models including non-Hodgkins lymphoma, pediatric glioma, small-cell carcinoma of the ovary, and synovial sarcomas. Tazemetostat has also been shown to control inflammatory genes by modulating IRF1, IRF8, and STAT1 levels suggesting therapeutic potential for the treatment of neuroinflammatory diseases associated with microglial activation.

    Purity

    >98 %

    Formula

    C34H44N4O4

    Solubility

    Soluble in DMSO (up to at least 25 mg/ml)
  • Restrictions

    For Research Use only
  • Format

    Powder

    Storage

    -20 °C
  • Background

    EPZ-6438,Transcription,Epigenetics,Proliferation,Protein methyltransferase,Cancer stem cells,Inflammation,Cancer,Posttranslational modification,Neurodegeneration,Chromatin

    Molecular Weight

    572.75

    CAS-No

    1403254-99-8
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